Stabilized antibody compositions

Abstract

The invention provides novel compositions of antibodies based on liquid vehicles selected from semifluorinated alkanes. The use of these vehicles provides for improved stability and shelf-life of antibodies and their derivatives. The compositions are useful for topical administration or for parenteral injection.

The invention claimed is: 
     
       1. A composition comprising an antigen-binding polypeptide or protein and a liquid vehicle, wherein the liquid vehicle comprises a semifluorinated alkane selected from F4H5, F4H6, F4H8, F6H4, F6H6, F6H8, and F6H10; and wherein the antigen-binding polypeptide or protein is incorporated in the composition such as to form a suspension;
 wherein the composition is substantially free of water. 
 
     
     
       2. The composition of  claim 1 , wherein the antigen-binding polypeptide or protein is selected from a monoclonal antibody, polyclonal antibody, an antibody fragment, a fusion protein comprising an antibody fragment, an antibody-drug conjugate, or any combination thereof. 
     
     
       3. The composition of  claim 2 , wherein the antibody fragment is a fragment antigen-binding (Fab), a single-chain variable fragment (scFv), a single-domain antibody, a minibody, or a diabody. 
     
     
       4. The composition of  claim 2 , wherein the monoclonal antibody is a chimeric, humanized, or human antibody. 
     
     
       5. The composition of  claim 1 , wherein the antigen-binding polypeptide or protein has a molecular mass of at least 90 kDa. 
     
     
       6. The composition of  claim 1 , wherein the semifluorinated alkane is selected from F4H5, F4H6, F4H8, F6H4, F6H6, and F6H8. 
     
     
       7. The composition of  claim 1 , wherein the semifluorinated alkane is selected from F4H5 and F6H8. 
     
     
       8. The composition of  claim 1 , wherein the semifluorinated alkane is F6H10. 
     
     
       9. The composition of  claim 1 , wherein the composition consists essentially of the antigen-binding polypeptide or protein and the liquid vehicle, the liquid vehicle consisting of one or more semi-fluorinated alkanes selected from F4H5, F4H6, F4H8, F6H4, F6H6, F6H8, and F6H10. 
     
     
       10. The composition of  claim 1 , wherein the composition retains at least 85% of its initial antigen-binding activity during storage of 6 months at a temperature of between RT to 40° C. 
     
     
       11. The composition of  claim 1 , wherein the antigen-binding polypeptide or protein is at a concentration of at least 0.5 mg/mL. 
     
     
       12. The composition of  claim 1 , wherein the antigen-binding polypeptide or protein is an angiogenesis inhibitor, an anti-proliferative agent or a TNF inhibitor. 
     
     
       13. The composition of  claim 2 , wherein the semifluorinated alkane is selected from F4H5, F4H6, F4H8, F6H4, F6H6, and F6H8. 
     
     
       14. The composition of  claim 13 , wherein the composition consists essentially of the antigen-binding polypeptide or protein and the liquid vehicle, the liquid vehicle consisting of one or more semi-fluorinated alkanes selected from F4H5 and F6H8. 
     
     
       15. The composition of  claim 13 , wherein the composition consists essentially of the antigen-binding polypeptide or protein and the liquid vehicle, the liquid vehicle consisting of F6H10. 
     
     
       16. The composition according to  claim 1 , wherein the antigen-binding polypeptide or protein is not dissolved in the SFA. 
     
     
       17. The composition according to  claim 1 , wherein the composition is formulated for topical administration to the eye, ear or nose or for parenteral administration. 
     
     
       18. The composition according to  claim 1 , wherein the antigen-binding polypeptide or protein is suspended as solid particles in the liquid vehicle. 
     
     
       19. The composition according to  claim 18 , wherein the solid particles of the antigen-binding polypeptide or protein are prepared by lyophilization or spray-drying of an aqueous or non-aqueous solution comprising the antigen-binding polypeptide or protein. 
     
     
       20. The composition according to  claim 18 , wherein the particle size of the suspended antigen-binding polypeptide or protein is adjusted before or after the particles are combined with the liquid vehicle.